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[CAS NO. 918407-35-9] Avoralstat
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-16735 |
| Brand: | MCE |
| CAS: | 918407-35-9 |
Overview
| MDL | MFCD28502152 |
|---|---|
| Molecular Weight | 513.54 |
| Molecular Formula | C28H27N5O5 |
| SMILES | O=C(C1=NC(C(NCC2CC2)=O)=CC=C1C3=CC(OC)=C(C=C)C=C3C(NC4=CC=C(C(N)=N)C=C4)=O)O |
4 Publications Citing Use of MCE
Summary
In Vitro
C1 inhibitor (C1INH) is the primary regulator of contact activation, both by inhibiting the conversion of prekallikrein to plasma kallikrein (PKK) by FXIIa, and by directly inhibiting PKK. PKK cleaves high molecular weight kininogen, releasing bradykinin, whose actions are responsible for the signs and symptoms of hereditary angioedema (HAE) [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02218294 | BioCryst Pharmaceuticals |
Hereditary Angioedema
|
August 2014 | Phase 1 |
| NCT02303626 | BioCryst Pharmaceuticals |
Hereditary Angioedema|HAE
|
November 2014 | Phase 2|Phase 3 |
| NCT02670720 | BioCryst Pharmaceuticals |
Hereditary Angioedema|HAE
|
December 2015 | Phase 3 |
| NCT01984788 | BioCryst Pharmaceuticals |
Hereditary Angioedema
|
November 2013 | Phase 2 |
| NCT02125162 | BioCryst Pharmaceuticals |
Hereditary Angioedema
|
April 2014 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 97.36 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9473 mL | 9.7363 mL | 19.4727 mL |
| 5 mM | 0.3895 mL | 1.9473 mL | 3.8945 mL |
| 10 mM | 0.1947 mL | 0.9736 mL | 1.9473 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution
References
- [1] Aygoren-Pursun E, et al. Prophylaxis of hereditary angioedema attacks: A randomized trial of oral plasma kallikrein inhibition with avoralstat. J Allergy Clin Immunol. 2016 Sep;138(3):934-936.e5.
- [2] Cornpropst M, et al. Safety, pharmacokinetics, and pharmacodynamics of avoralstat, an oral plasma kallikrein inhibitor: phase 1 study. Allergy. 2016;71(12):1676-1683.
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